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    Oral Medicament Based on a Proton Pump Inhibitor
    1.
    发明申请
    Oral Medicament Based on a Proton Pump Inhibitor 审中-公开
    基于质子泵抑制剂的口服药物

    公开(公告)号：US20100068291A1

    公开(公告)日：2010-03-18

    申请号：US11920278

    申请日：2006-05-15

    申请人： Philippe CAISSE ,  Catherine CASTAN ,  Rémi MEYRUEIX ,  Gérard SOULA

    发明人： Philippe CAISSE ,  Catherine CASTAN ,  Rémi MEYRUEIX ,  Gérard SOULA

    IPC分类号： A61K9/50 ,  A61K31/4439 ,  A61K31/426 ,  A61K31/4164 ,  A61K31/341 ,  A61K47/02 ,  A61K47/06

    CPC分类号： A61K9/5047 ,  A61K9/5015 ,  A61K9/5026 ,  A61K31/00 ,  A61K31/4184 ,  A61K31/4439

    摘要： The invention relates to oral medicaments having a modified release of proton pump inhibitors (PPI's) that are, in particular, useful in preventing and treating gastrointestinal disorders. The aim of the invention is to provide a novel oral medicament based on PPI's ideally having all or some of the following characteristics: a) quickly providing relief to the patient by increasing the gastric pH after oral administration of the medicament; b) accelerating the recovery of patients while maintaining this increase in the gastric pH for as long as possible after oral administration of the medicament and, in particular, during the night; c) improving the observance of the treatment and the comfort of the patient by taking the medicament once daily. To this end, the microcapsules of the invention, preferably non-enteric, are constituted of PPI microparticles coated with ethyl cellulose, an ammonio methacrylate copolymer (Eudragit® RL 100), polyvinylpyrrolidone, castor oil and polyoxyethylenated hydrogenated castor oil (40). This medicament is designed so that after its ingestion for a once daily administration, it makes it possible to maintain, from the first day of treatment onward, an average gastric pH, between 0 and 24 h, of greater than or equal to the average gastric pH between 0 and 24 h obtained by an enteric oral medicament having a reference* immediate release, administered under the same conditions. The invention also relates to these microcapsules per se.

    摘要翻译： 本发明涉及具有特别可用于预防和治疗胃肠道疾病的质子泵抑制剂（PPI's）的改良释放的口服药物。 本发明的目的是提供一种基于PPI的新型口服药物，其理想地具有以下所有或一些特征：a）通过在口服给药药物后增加胃pH，快速地向患者提供缓解; b）加速患者的恢复，同时在药物口服给药后，尽可能长时间地保持胃pH的增加，特别是在夜间; c）通过每天服用一次药物来改善患者的治疗和舒适度。 为此，本发明的微胶囊优选为非肠溶性，由涂覆有乙基纤维素的PPI微粒，氨基甲基丙烯酸共聚物（RL100），聚乙烯吡咯烷酮，蓖麻油和聚氧乙烯化氢化蓖麻油（40）构成。 这种药物被设计成使其在摄入一次每日给药后，可以从治疗的第一天开始维持0至24小时之间的平均胃pH大于或等于胃平均值 通过具有参考*立即释放的肠溶口服药物在相同条件下给药获得的0至24小时的pH。 本发明还涉及这些微胶囊本身。